Contraindicated in:
Use Cautiously in:
CV: hypertension, chest pain.
Derm: rash.
GI: diarrhea, nausea, ↑ liver enzymes, abdominal pain, HEPATOTOXICITY.
GU: ↓ fertility (females).
Hemat: NEUTROPENIA.
Neuro: dizziness, fatigue.
Drug-Drug:
Absorption: Prodrug that is converted to an active metabolite, R406; absolute bioavailability of R406 is 55%; absorption enhanced by high-calorie, high-fat foods.
Distribution: Extensively distributed to tissues.
Metabolism/Excretion: Metabolized in the gut by alkaline phosphatase to its major active metabolite, R406. R406 primarily metabolized in liver by CYP3A4 isoenzyme and through glucuronidation by UGT1A9. 80% of R406 excreted in feces, 20% in urine.
Half-life: R406: 15 hr.
NDC Code*